PTPN13
gene geneOn this page
Also known as PTP1EPTP-BASPTPL1PTP-BL
Summary
PTPN13 (protein tyrosine phosphatase non-receptor type 13, HGNC:9646) is a protein-coding gene on chromosome 4q21.3, encoding Tyrosine-protein phosphatase non-receptor type 13 (Q12923). Tyrosine phosphatase which negatively regulates FAS-induced apoptosis and NGFR-mediated pro-apoptotic signaling.
The protein encoded by this gene is a member of the protein tyrosine phosphatase (PTP) family. PTPs are signaling molecules that regulate a variety of cellular processes including cell growth, differentiation, mitotic cycle, and oncogenic transformation. This PTP is a large intracellular protein. It has a catalytic PTP domain at its C-terminus and two major structural domains: a region with five PDZ domains and a FERM domain that binds to plasma membrane and cytoskeletal elements. This PTP was found to interact with, and dephosphorylate, Fas receptor and IkappaBalpha through the PDZ domains. This suggests it has a role in Fas mediated programmed cell death. This PTP was also shown to interact with GTPase-activating protein, and thus may function as a regulator of Rho signaling pathways. Four alternatively spliced transcript variants, which encode distinct proteins, have been reported.
Source: NCBI Gene 5783 — RefSeq curated summary.
At a glance
- Gene–disease (curated): bone marrow failure syndrome (Moderate, GenCC)
- GWAS associations: 7
- Clinical variants (ClinVar): 435 total
- Druggable target: yes
- Cancer driver (intOGen): loss-of-function (tumor-suppressor-like) across 3 cancer types
- MANE Select transcript:
NM_080683
Identifiers
Gene identifiers
| Field | Value |
|---|---|
| HGNC ID | HGNC:9646 |
| Approved symbol | PTPN13 |
| Name | protein tyrosine phosphatase non-receptor type 13 |
| Location | 4q21.3 |
| Locus type | gene with protein product |
| Status | Approved |
| Aliases | PTP1E, PTP-BAS, PTPL1, PTP-BL |
| Ensembl gene | ENSG00000163629 |
| Ensembl biotype | protein_coding |
| OMIM | 600267 |
| Entrez | 5783 |
Gene structure
Transcript identifiers
Ensembl transcripts: 24 — 22 protein_coding, 2 retained_intron
ENST00000316707, ENST00000411767, ENST00000427191, ENST00000436978, ENST00000502971, ENST00000507902, ENST00000508063, ENST00000511105, ENST00000511467, ENST00000860769, ENST00000860770, ENST00000860771, ENST00000860772, ENST00000940451, ENST00000940452, ENST00000940453, ENST00000940454, ENST00000940455, ENST00000940456, ENST00000940457, ENST00000940458, ENST00000940459, ENST00000953522, ENST00000953523
RefSeq mRNA: 4 — MANE Select: NM_080683
NM_006264, NM_080683, NM_080684, NM_080685
CCDS: CCDS47093, CCDS47094, CCDS47095, CCDS47096
Canonical transcript exons
ENST00000411767 — 48 exons
| Exon | Start | End |
|---|---|---|
| ENSE00001076725 | 86764593 | 86764724 |
| ENSE00001076728 | 86769769 | 86769983 |
| ENSE00001076729 | 86807560 | 86807897 |
| ENSE00001076731 | 86809769 | 86809984 |
| ENSE00001076736 | 86785848 | 86785936 |
| ENSE00001076737 | 86770101 | 86770199 |
| ENSE00001076740 | 86774373 | 86774531 |
| ENSE00001076741 | 86766432 | 86766517 |
| ENSE00001076747 | 86803709 | 86803857 |
| ENSE00001076749 | 86772778 | 86772958 |
| ENSE00001076752 | 86775442 | 86775652 |
| ENSE00001076758 | 86796874 | 86796929 |
| ENSE00001076761 | 86732592 | 86732766 |
| ENSE00001076763 | 86767817 | 86767976 |
| ENSE00001076767 | 86771171 | 86771535 |
| ENSE00001216640 | 86799101 | 86799204 |
| ENSE00001216712 | 86741634 | 86741816 |
| ENSE00001216802 | 86775171 | 86775342 |
| ENSE00001216927 | 86735594 | 86735746 |
| ENSE00001216934 | 86734737 | 86734875 |
| ENSE00001216943 | 86734303 | 86734456 |
| ENSE00001325693 | 86762727 | 86763190 |
| ENSE00001364834 | 86635252 | 86635371 |
| ENSE00001364860 | 86672365 | 86672543 |
| ENSE00001366520 | 86693587 | 86693674 |
| ENSE00001368206 | 86750470 | 86750887 |
| ENSE00001369928 | 86701241 | 86701801 |
| ENSE00001371682 | 86732400 | 86732474 |
| ENSE00001372823 | 86716530 | 86716625 |
| ENSE00001377593 | 86717024 | 86717117 |
| ENSE00001382188 | 86722212 | 86722434 |
| ENSE00001387588 | 86689005 | 86689190 |
| ENSE00001388101 | 86686710 | 86686775 |
| ENSE00001390951 | 86744966 | 86745128 |
| ENSE00001403980 | 86805279 | 86805369 |
| ENSE00001406653 | 86753009 | 86753065 |
| ENSE00001407850 | 86758678 | 86758785 |
| ENSE00001415404 | 86780402 | 86780472 |
| ENSE00001416845 | 86594315 | 86594789 |
| ENSE00001417450 | 86811046 | 86811108 |
| ENSE00001420498 | 86751027 | 86751124 |
| ENSE00001421731 | 86758260 | 86758349 |
| ENSE00001428369 | 86782201 | 86782262 |
| ENSE00001797192 | 86785231 | 86785368 |
| ENSE00001804791 | 86784465 | 86784558 |
| ENSE00003460634 | 86765395 | 86765488 |
| ENSE00003559640 | 86758942 | 86759073 |
| ENSE00003845816 | 86814456 | 86815161 |
Expression profiles
Bgee: expression breadth ubiquitous, 286 present calls, max score 97.09.
FANTOM5 (CAGE): breadth ubiquitous, TPM avg 20.8890 / max 1049.0498, expressed in 1481 samples.
FANTOM5 promoters (2 alternative TSS)
| Promoter ID | TPM avg | Samples expressed |
|---|---|---|
| 48670 | 15.8503 | 1442 |
| 48671 | 5.0386 | 1185 |
Top tissues by expression
293 total, by Bgee expression score (0-100, higher = more expressed):
| Tissue | Anatomy ID | Expression score | Quality |
|---|---|---|---|
| mucosa of paranasal sinus | UBERON:0005030 | 97.09 | gold quality |
| urethra | UBERON:0000057 | 96.72 | gold quality |
| penis | UBERON:0000989 | 96.47 | gold quality |
| palpebral conjunctiva | UBERON:0001812 | 96.05 | gold quality |
| pigmented layer of retina | UBERON:0001782 | 95.88 | gold quality |
| upper arm skin | UBERON:0004263 | 95.86 | gold quality |
| renal medulla | UBERON:0000362 | 95.64 | gold quality |
| trigeminal ganglion | UBERON:0001675 | 95.33 | gold quality |
| endometrium epithelium | UBERON:0004811 | 94.77 | gold quality |
| gingival epithelium | UBERON:0001949 | 94.71 | gold quality |
| gingiva | UBERON:0001828 | 94.59 | gold quality |
| pharyngeal mucosa | UBERON:0000355 | 94.23 | gold quality |
| calcaneal tendon | UBERON:0003701 | 94.03 | gold quality |
| dorsal root ganglion | UBERON:0000044 | 93.73 | gold quality |
| cervix squamous epithelium | UBERON:0006922 | 93.38 | gold quality |
| upper leg skin | UBERON:0004262 | 93.31 | gold quality |
| cervix epithelium | UBERON:0004801 | 93.28 | gold quality |
| epithelium of nasopharynx | UBERON:0001951 | 93.11 | gold quality |
| corpus callosum | UBERON:0002336 | 93.01 | gold quality |
| skin of hip | UBERON:0001554 | 91.65 | gold quality |
| choroid plexus epithelium | UBERON:0003911 | 91.65 | gold quality |
| skin of abdomen | UBERON:0001416 | 91.62 | gold quality |
| oral cavity | UBERON:0000167 | 91.25 | gold quality |
| zone of skin | UBERON:0000014 | 91.22 | gold quality |
| nasal cavity epithelium | UBERON:0005384 | 91.06 | gold quality |
| skin of leg | UBERON:0001511 | 90.97 | gold quality |
| tongue squamous epithelium | UBERON:0006919 | 90.78 | gold quality |
| mammalian vulva | UBERON:0000997 | 90.77 | gold quality |
| corpus epididymis | UBERON:0004359 | 90.64 | gold quality |
| lower lobe of lung | UBERON:0008949 | 90.33 | gold quality |
Single-cell (SCXA)
Detected in 4 experiment(s), a significant marker in 3.
| Experiment | Marker? | Max mean expression |
|---|---|---|
| E-CURD-119 | yes | 37.27 |
| E-GEOD-130148 | yes | 12.76 |
| E-CURD-112 | no | 2.99 |
| E-ANND-3 | no | 0.00 |
Regulation
Is transcription factor: no
Upstream regulators (CollecTRI, top): CEBPB, CUX1, ETV6, EWSR1, FLI1, FOXC1, IRF8, NFKB1, NFKB, RELA, SPI1, STAT3, TP53
miRNA regulators (miRDB)
88 targeting PTPN13, top 30 by miRDB confidence (max_score; target_count = how many genes the miRNA targets in total — lower means more specific):
| miRNA | Max score | Avg score | miRNA target_count |
|---|---|---|---|
| HSA-MIR-30A-5P | 100.00 | 76.31 | 3233 |
| HSA-MIR-30B-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30C-5P | 100.00 | 76.29 | 3248 |
| HSA-MIR-30D-5P | 100.00 | 76.32 | 3233 |
| HSA-MIR-30E-5P | 100.00 | 76.32 | 3242 |
| HSA-MIR-1277-5P | 100.00 | 73.95 | 5056 |
| HSA-MIR-3163 | 100.00 | 77.23 | 8605 |
| HSA-MIR-656-3P | 100.00 | 72.15 | 2788 |
| HSA-MIR-5692A | 100.00 | 74.40 | 6850 |
| HSA-MIR-200B-3P | 100.00 | 73.31 | 2693 |
| HSA-MIR-200C-3P | 100.00 | 73.35 | 2685 |
| HSA-MIR-429 | 100.00 | 73.44 | 2698 |
| HSA-MIR-548C-3P | 99.99 | 74.01 | 7587 |
| HSA-MIR-4282 | 99.99 | 75.36 | 6408 |
| HSA-MIR-520D-5P | 99.98 | 73.34 | 4883 |
| HSA-MIR-524-5P | 99.98 | 73.43 | 4882 |
| HSA-MIR-548N | 99.98 | 71.94 | 4170 |
| HSA-MIR-12136 | 99.98 | 72.81 | 5713 |
| HSA-MIR-3148 | 99.97 | 75.06 | 6478 |
| HSA-MIR-5688 | 99.96 | 73.23 | 4504 |
| HSA-MIR-495-3P | 99.96 | 72.81 | 4197 |
| HSA-MIR-9-3P | 99.96 | 70.88 | 2068 |
| HSA-MIR-101-3P | 99.94 | 75.03 | 2230 |
| HSA-MIR-144-3P | 99.94 | 73.98 | 2698 |
| HSA-MIR-335-3P | 99.93 | 73.36 | 4958 |
| HSA-MIR-7-1-3P | 99.91 | 71.53 | 4384 |
| HSA-MIR-7-2-3P | 99.91 | 71.40 | 4394 |
| HSA-MIR-1297 | 99.91 | 73.41 | 3162 |
| HSA-MIR-3121-3P | 99.82 | 71.96 | 3630 |
| HSA-MIR-4307 | 99.82 | 70.45 | 3374 |
Literature-anchored findings (GeneRIF, showing 40)
- Structure, dynamics and binding characteristics of the second PDZ domain of PTP-BL (PMID:11884147)
- expression and apoptosis induction in peripheral blood cells from liver graft (PMID:11959286)
- PDZ2 domain from cytosolic human phosphatase hPTP1E complexed with peptide, RA-GEF-2, reveals contribution of the beta2-beta3 loop to PDZ domain-ligand interactions (PMID:12095257)
- PTPL1/FAP-1 has a key role in the apoptotic process in human breast cancer cells independent of Fas but associated with an early inhibition of the insulin receptor substrate-1/phosphatidylinositol 3-kinase pathway (PMID:12354757)
- Shares a promoter region with the tightly linked gene encoding stress-activated protein kinase JNK3. (PMID:12436199)
- FAP-1 has a role in binding to, and consequently inhibition of, Fas export to the cell surface (PMID:12724420)
- specificity of interaction between the second PDZ domain of human protein tyrosine phosphatase1E (PDZ2) and a C-terminal peptide, ENEQVSAV, from the guanine nucleotide exchange factor RA-GEF-2 was investigated using FTIR spectroscopy and ESI-MS (PMID:12870871)
- PTPL1 binds to tandem-PH-domain-containing protein (TAPP)-1. (PMID:14516276)
- Data report the solution structure of the PDZ2 domain splicing variant of the protein tyrosine phosphatase PTP-Bas. (PMID:14596806)
- X-ray crystallographic analysis of the PTPL1 catalytic domain (PMID:15611135)
- We therefore report a novel transcriptional activation of a phosphatase involved in the oncogenesis of ESFT. (PMID:15782144)
- FAP-1 expression is often up-regulated in metastatic tumors, with a causal connection withNF-kappaB-dependent transcriptional regulation of FAP-1 gene expression. (PMID:16306044)
- FAP-1 could be inactivated during hepatocarcinogenesis, mainly attributed by allelic loss and promoter methylation. (PMID:16489062)
- The PTPN13 protein has proapoptotic functions and can fuction as TSGs to suppress tumorigenesis. (PMID:16572203)
- FAP-1 phosphatase activity could be responsible for NF-kappaB activation and resistance of SCCHN cells to Fas-mediated apoptosis. (PMID:16888780)
- use the second PDZ domain (PDZ2) of protein tyrosine phosphatase (PTP1E) as a model to study the energetics of peptide binding to a class I PDZ domain. (PMID:17240990)
- PTPN13/PTPL1 induces apoptosis through insulin receptor substrate-1 dephosphorylation (PMID:17638892)
- cellular PTPN13 inhibits Her2 activity by dephosphorylating the signal domain of Her2 and plays a role in attenuating invasiveness and metastasis of Her2 overactive tumors. (PMID:17982484)
- Frameshift mutation in the polyadenine tracts in both FLASH and PTPN13 genes is rare in colorectal carcinomas. Both FLASH and PTPN13 mutations in the polyadenine tracts may not have a crucial role in the pathogenesis of colorectal carcinomas. (PMID:18038312)
- The interferon consensus sequence-binding protein (ICSBP/IRF8) represses PTPN13 gene transcription in differentiating myeloid cells (PMID:18195016)
- erythrocyte CR1 ligation induces its clustering in complex with scaffolding protein FAP-1 (PMID:18684861)
- PTPL1 expression level is an independent prognostic indicator of favorable outcome for patients with breast cancer (PMID:19004008)
- PTPN13 SNPs were found to influence susceptibility to a wide spectrum of cancers. (PMID:19672627)
- PTPN13 phosphatase activity has a physiologically significant role in regulating MAP kinase signaling (PMID:19734941)
- polymorphisms in the PTPN13 coding region may have a role in susceptibility to squamous cell carcinoma of head and neck (PMID:19892796)
- Transfection of FAP-1 siRNA into SW480 cells silenced the expression of FAP-1 and consequently abolished the inhibitory function of Fas/FasL-mediated apoptosis pathway, thus increasing the efficacy of chemotherapy for colon carcinoma with oxaliplatin. (PMID:20039457)
- PTPL1 regulates breast cancer cell aggressiveness through direct inactivation of Src kinase. (PMID:20501847)
- FAP-1 was demonstrated to be responsible for the reduced sensitivity to CD95-mediated apoptosis in cells with inhibited miR-200. (PMID:20620960)
- X-ray crystal structures of PDZ2 in the absence and presence of RA-GEF2 ligand; very minor structural changes in PDZ2 accompany peptide binding (PMID:20839809)
- REVIEW: the alterations in expression and the genetic and epigenetic arguments supporting an oncogenic or an anti-oncogenic impact of PTPL1 (PMID:21235435)
- The Ret oncoprotein exerts opposing controls on Fap-1 and CD95, increasing Fap-1 expression and decreasing CD95 cell surface expression. (PMID:21741956)
- interaction between Tel and Tel-PdgfRbeta decreases Tel/Icsbp/Hdac3 binding to the PTPN13 cis element, resulting in increased transcription. (PMID:22262849)
- The PTPL1 is an important mediator of central cellular processes such as proliferation and invasion. (PMID:22274591)
- Data show that EphrinB1, a PTPN13 substrate, interacts with ErbB2, and Src kinase mediates EphrinB1 phosphorylation and subsequent MAP Kinase signaling. (PMID:22279592)
- CD95 signal transduction was not affected by FAP-1 expression in A818-6 monolayer cells; we found a polarisation-induced co-localisation of CD95 and FAP-1. (PMID:22364882)
- Studied the peptide binding induced dynamical changes at the side-chain level throughout the second PDZ domain of PTP1e, identifying as such the collection of residues involved in long-range communication. (PMID:23209399)
- Fap1-dependent inactivation of Gsk3beta and consequent stabilization of betacatenin in these cells. Consistent with this, Bcr-abl(+) cells exhibited a Fap1-dependent increase in betacatenin activity. (PMID:23519466)
- The loss of PTPL1 and PKC-delta expression in poorly differentiated, more aggressive human prostate cancers indicate that their absence could be related to apoptosis resistance and tumor progression. (PMID:23559010)
- PTPL1 dephosphorylates p85beta, promoting its binding to FBXL2 and degradation. (PMID:23604317)
- Low PTPN13 expression is associated with invasion and metastasis of lung squamous cell carcinoma. (PMID:23906871)
Cross-species orthologs
3 orthologs
| Organism | Symbol | Gene ID |
|---|---|---|
| danio_rerio | ptpn13 | ENSDARG00000103699 |
| mus_musculus | Ptpn13 | ENSMUSG00000034573 |
| rattus_norvegicus | Ptpn13 | ENSRNOG00000002061 |
Paralogs (35): PTPRN (ENSG00000054356), PTPRU (ENSG00000060656), PTPN3 (ENSG00000070159), PTPN21 (ENSG00000070778), PTPN18 (ENSG00000072135), PTPN23 (ENSG00000076201), PTPRH (ENSG00000080031), PTPRC (ENSG00000081237), PTPN4 (ENSG00000088179), PTPRS (ENSG00000105426), PTPRZ1 (ENSG00000106278), PTPN5 (ENSG00000110786), PTPN6 (ENSG00000111679), PTPRB (ENSG00000127329), PTPN12 (ENSG00000127947), PTPRE (ENSG00000132334), PTPRA (ENSG00000132670), PTPN22 (ENSG00000134242), PTPRF (ENSG00000142949), PTPN7 (ENSG00000143851), PTPRG (ENSG00000144724), PTPRJ (ENSG00000149177), PTPRO (ENSG00000151490), PTPN14 (ENSG00000152104), PTPRK (ENSG00000152894), PTPRR (ENSG00000153233), PTPRD (ENSG00000153707), PTPRN2 (ENSG00000155093), PTPN9 (ENSG00000169410), PTPRM (ENSG00000173482), PTPN2 (ENSG00000175354), PTPN11 (ENSG00000179295), PTPRT (ENSG00000196090), PTPN1 (ENSG00000196396), PTPN20 (ENSG00000204179)
Protein
Protein identifiers
Tyrosine-protein phosphatase non-receptor type 13 — Q12923 (reviewed: Q12923)
Alternative names: Fas-associated protein-tyrosine phosphatase 1, PTP-BAS, Protein-tyrosine phosphatase 1E, Protein-tyrosine phosphatase PTPL1
All UniProt accessions (3): Q12923, D6R9M4, D6R9X4
UniProt curated annotations — full annotation on UniProt →
Function. Tyrosine phosphatase which negatively regulates FAS-induced apoptosis and NGFR-mediated pro-apoptotic signaling. May regulate phosphoinositide 3-kinase (PI3K) signaling through dephosphorylation of PIK3R2.
Subunit / interactions. Interacts (via the first PDZ domain) with PLEKHA1 and PLEKHA2. Interacts (via the second PDZ domain) with TNFRSF6 (Fas receptor) (via C-terminus). Interacts (via the second PDZ domain) with TRIP6 (via the third LIM domain and C-terminus). Interacts (via the third PDZ domain) with NGFR (via C-terminal SVP motif) and PKN2 (via C-terminus). Interacts (via the second or fourth PDZ domains) with PDLIM4 (via C-terminus only or via combined C-terminus and LIM domain, but not LIM domain only). Found in a complex with PDLIM4 and TRIP6. Interacts with PDLIM4; this interaction results in dephosphorylation of SRC ‘Tyr-419’ by this protein leading to its inactivation. Interacts with BRD7. Interacts with RAPGEF6. Interacts with ARHGAP29. Interacts with PIK3R2; dephosphorylates PIK3R2. Interacts with FBXL2. Interacts (via the FERM domain) with ENTR1. Found in a complex with ENTR1, PTPN13 and GIT1.
Subcellular location. Cytoplasm. Cytoskeleton. Nucleus. Cell projection. Lamellipodium.
Tissue specificity. Expressed in keratinocytes (at protein level). Present in most tissues with the exception of the liver and skeletal muscle. Most abundant in lung, kidney and fetal brain.
Miscellaneous. May be due to a competing donor splice site.
Similarity. Belongs to the protein-tyrosine phosphatase family. Non-receptor class subfamily.
Isoforms (4)
| UniProt ID | Names | Canonical? |
|---|---|---|
| Q12923-1 | 1 | yes |
| Q12923-2 | 2 | |
| Q12923-3 | 3 | |
| Q12923-4 | 4 |
RefSeq proteins (4): NP_006255, NP_542414, NP_542415, NP_542416 (=MANE)
Domains & families (InterPro)
| ID | Name | Type |
|---|---|---|
| IPR000242 | PTP_cat | Domain |
| IPR000299 | FERM_domain | Domain |
| IPR000387 | Tyr_Pase_dom | Domain |
| IPR001478 | PDZ | Domain |
| IPR003595 | Tyr_Pase_cat | Domain |
| IPR011019 | KIND_dom | Domain |
| IPR011993 | PH-like_dom_sf | Homologous_superfamily |
| IPR012153 | PTPN13 | Family |
| IPR014352 | FERM/acyl-CoA-bd_prot_sf | Homologous_superfamily |
| IPR018979 | FERM_N | Domain |
| IPR018980 | FERM_PH-like_C | Domain |
| IPR019748 | FERM_central | Domain |
| IPR019749 | Band_41_domain | Domain |
| IPR029021 | Prot-tyrosine_phosphatase-like | Homologous_superfamily |
| IPR029071 | Ubiquitin-like_domsf | Homologous_superfamily |
| IPR035963 | FERM_2 | Homologous_superfamily |
| IPR036034 | PDZ_sf | Homologous_superfamily |
| IPR052074 | NonRcpt_TyrProt_Phosphatase | Family |
Pfam: PF00102, PF00373, PF00595, PF09379, PF09380, PF16599
Enzyme classification (BRENDA):
- EC 3.1.3.48 — protein-tyrosine-phosphatase (BRENDA: 59 organisms, 501 substrates, 1326 inhibitors, 270 Km, 165 kcat entries)
Substrate kinetics (BRENDA)
70 substrates with measured Km, best-characterized 15. Km ranges are aggregated across organisms/conditions.
| Substrate | Km (mM) | Measurements |
|---|---|---|
| 4-NITROPHENYL PHOSPHATE | 0.0008–148 | 84 |
| 6,8-DIFLUORO-4-METHYLUMBELLIFERYL PHOSPHATE | 0.0039–0.862 | 27 |
| P-NITROPHENYL PHOSPHATE | 0.0024–10 | 20 |
| DADEPYLIPQQG | 0.0003–0.1 | 12 |
| PHOSPHOTYROSINE | 0.012–30 | 11 |
| LYSOZYME | 0.0003–0.012 | 5 |
| MYELIN BASIC PROTEIN | 0.0001–0.022 | 5 |
| ACETYL-DADEPY-NH2 | 0.0228–0.219 | 4 |
| ACETYL-DADEPYL-NH2 | 1.1–97.5 | 4 |
| 4,6,8-TRIMETHYL-2-OXO-2H-CHROMEN-7-YL DIHYDROGEN | 0.02–0.156 | 3 |
| SASASPYSASA | 0.53–2.3 | 3 |
| 1-NAPHTHYL PHOSPHATE | 1.19–1.88 | 2 |
| 3,6-FLUORESCEIN DIPHOSPHATE | 15–19 | 2 |
| 4-METHYLUMBELLIFERYL PHOSPHATE | 0.953–2.41 | 2 |
| BOVINE SERUM ALBUMIN | 0.0001–0.0003 | 2 |
Catalyzed reactions (Rhea), 1 shown:
- O-phospho-L-tyrosyl-[protein] + H2O = L-tyrosyl-[protein] + phosphate (RHEA:10684)
UniProt features (123 total): strand 23, helix 16, compositionally biased region 12, sequence conflict 12, region of interest 11, modified residue 11, mutagenesis site 11, domain 8, sequence variant 7, turn 3, binding site 3, splice variant 3, chain 1, coiled-coil region 1, active site 1
Structure
Experimental structures (PDB)
12 structures.
| PDB | Method | Resolution (Å) |
|---|---|---|
| 3LNY | X-RAY DIFFRACTION | 1.3 |
| 5GLJ | X-RAY DIFFRACTION | 1.6 |
| 3LNX | X-RAY DIFFRACTION | 1.64 |
| 1WCH | X-RAY DIFFRACTION | 1.85 |
| 7XTY | X-RAY DIFFRACTION | 2.1 |
| 1D5G | SOLUTION NMR | |
| 1Q7X | SOLUTION NMR | |
| 2M0Z | SOLUTION NMR | |
| 2M10 | SOLUTION NMR | |
| 3PDZ | SOLUTION NMR | |
| 7QCX | SOLUTION NMR | |
| 7QCY | SOLUTION NMR |
Predicted structure (AlphaFold)
| Model | pLDDT | Fraction very-high |
|---|---|---|
| AF-Q12923-F1 | 60.36 | 0.21 |
Functional residue map
Curated UniProt residues grouped by drug-discovery relevance — catalytic, ligand-binding, modification, and mutation-validated positions. Source: UniProtKB sequence features.
Catalytic / active sites (1): 2408 (phosphocysteine intermediate)
Ligand- & substrate-binding residues (3): 2378; 2408–2414; 2452
Post-translational modifications (11): 240, 301, 302, 890, 897, 908, 911, 914, 1029, 1033, 1085
Mutagenesis-validated functional residues (11):
| Position | Phenotype |
|---|---|
| 2154 | no effect on substrate affinity. |
| 2205 | no effect on substrate affinity. |
| 2221 | reduces substrate affinity 2 fold. |
| 2307 | reduces substrate affinity 7 fold. |
| 2408 | loss of catalytic activity. |
| 2444 | loss of catalytic activity. |
| 2444 | reduces substrate affinity 7 fold. |
| 2444 | strongly decreases catalytic activity. |
| 2448 | reduces substrate affinity 2 fold. |
| 2449 | loss of catalytic activity. |
| 2474 | no effect on substrate affinity. |
Function
Pathways and Gene Ontology
Reactome pathways
5 pathways
| ID | Pathway |
|---|---|
| R-HSA-1660499 | Synthesis of PIPs at the plasma membrane |
| R-HSA-9008059 | Interleukin-37 signaling |
| R-HSA-9696264 | RND3 GTPase cycle |
| R-HSA-9696270 | RND2 GTPase cycle |
| R-HSA-9696273 | RND1 GTPase cycle |
MSigDB gene sets: 315 (showing top):
GOBP_REGULATION_OF_PHOSPHORYLATION, REACTOME_CYTOKINE_SIGNALING_IN_IMMUNE_SYSTEM, GOBP_SYNAPSE_ASSEMBLY, GOZGIT_ESR1_TARGETS_DN, LINDGREN_BLADDER_CANCER_CLUSTER_3_DN, GOBP_REGULATION_OF_CELL_JUNCTION_ASSEMBLY, GOBP_NEGATIVE_REGULATION_OF_CELL_JUNCTION_ASSEMBLY, GOBP_REGULATION_OF_NERVOUS_SYSTEM_DEVELOPMENT, GOBP_REGULATION_OF_CELLULAR_COMPONENT_BIOGENESIS, GOBP_NEGATIVE_REGULATION_OF_NERVOUS_SYSTEM_DEVELOPMENT, GOBP_NEGATIVE_REGULATION_OF_CELLULAR_COMPONENT_ORGANIZATION, MARTINEZ_RB1_TARGETS_UP, GOBP_NEGATIVE_REGULATION_OF_MULTICELLULAR_ORGANISMAL_PROCESS, GOBP_CELL_JUNCTION_ORGANIZATION, GOBP_CELLULAR_RESPONSE_TO_TOXIC_SUBSTANCE
GO Biological Process (8): negative regulation of protein phosphorylation (GO:0001933), protein dephosphorylation (GO:0006470), peptidyl-tyrosine dephosphorylation (GO:0035335), regulation of phosphatidylinositol 3-kinase/protein kinase B signal transduction (GO:0051896), cellular response to toxic substance (GO:0097237), negative regulation of excitatory synapse assembly (GO:1904890), dephosphorylation (GO:0016311), regulatory ncRNA-mediated gene silencing (GO:0031047)
GO Molecular Function (5): protein tyrosine phosphatase activity (GO:0004725), phosphatidylinositol 3-kinase regulatory subunit binding (GO:0036312), phosphoprotein phosphatase activity (GO:0004721), protein binding (GO:0005515), hydrolase activity (GO:0016787)
GO Cellular Component (9): nucleus (GO:0005634), nucleoplasm (GO:0005654), cytoplasm (GO:0005737), cytoskeleton (GO:0005856), plasma membrane (GO:0005886), lamellipodium (GO:0030027), cell body (GO:0044297), extracellular exosome (GO:0070062), cell projection (GO:0042995)
Reactome top-level categories
Rollup of top-3 pathways:
| Category | Pathways |
|---|---|
| RHO GTPase cycle | 3 |
| PI Metabolism | 1 |
| Interleukin-1 family signaling | 1 |
GO top-level categories
Rollup of top GO terms by namespace:
| Category | Terms |
|---|---|
| cellular anatomical structure | 4 |
| regulation of protein phosphorylation | 1 |
| protein phosphorylation | 1 |
| negative regulation of protein modification process | 1 |
| negative regulation of phosphorylation | 1 |
| dephosphorylation | 1 |
| protein modification process | 1 |
| protein dephosphorylation | 1 |
| phosphatidylinositol 3-kinase/protein kinase B signal transduction | 1 |
| regulation of intracellular signal transduction | 1 |
| response to toxic substance | 1 |
| cellular response to chemical stimulus | 1 |
| negative regulation of synapse assembly | 1 |
| excitatory synapse assembly | 1 |
| regulation of excitatory synapse assembly | 1 |
| phosphate-containing compound metabolic process | 1 |
| negative regulation of gene expression | 1 |
| phosphoprotein phosphatase activity | 1 |
| phosphatidylinositol 3-kinase binding | 1 |
| phosphatase activity | 1 |
| catalytic activity, acting on a protein | 1 |
| binding | 1 |
| catalytic activity | 1 |
| intracellular membrane-bounded organelle | 1 |
| nuclear lumen | 1 |
| intracellular anatomical structure | 1 |
| intracellular membraneless organelle | 1 |
| membrane | 1 |
| cell periphery | 1 |
| cell leading edge | 1 |
| plasma membrane bounded cell projection | 1 |
| extracellular vesicle | 1 |
Protein interactions and networks
STRING
1457 interactions, top by confidence (×1000):
| Protein A | Protein B | Partner UniProt | Score |
|---|---|---|---|
| PTPN13 | FAS | P25445 | 923 |
| PTPN13 | ARHGAP29 | Q52LW3 | 861 |
| PTPN13 | EFNB1 | P98172 | 825 |
| PTPN13 | RAPGEF6 | Q8TEU7 | 817 |
| PTPN13 | EFNB2 | P52799 | 764 |
| PTPN13 | EFNB3 | Q15768 | 725 |
| PTPN13 | CAV1 | Q03135 | 713 |
| PTPN13 | SRC | P12931 | 708 |
| PTPN13 | APC | P25054 | 682 |
| PTPN13 | PRY | O14603 | 682 |
| PTPN13 | PTPRG | P23470 | 633 |
| PTPN13 | ENTR1 | Q96C92 | 630 |
| PTPN13 | PTS | Q03393 | 621 |
| PTPN13 | EPHB4 | P54760 | 600 |
| PTPN13 | FADD | Q13158 | 592 |
| PTPN13 | PDCD10 | Q9BUL8 | 592 |
IntAct
654 interactions, top by confidence:
| A | B | Type | Score |
|---|---|---|---|
| PDCD10 | STK25 | psi-mi:“MI:0914”(association) | 0.980 |
| YWHAB | PIK3C2A | psi-mi:“MI:0914”(association) | 0.800 |
| RNF146 | TNKS | psi-mi:“MI:0914”(association) | 0.790 |
| RAPGEF1 | CRKL | psi-mi:“MI:0914”(association) | 0.720 |
| CFTR | ESYT2 | psi-mi:“MI:2364”(proximity) | 0.710 |
| E | PTPN13 | psi-mi:“MI:0915”(physical association) | 0.670 |
| PTPN13 | E | psi-mi:“MI:0915”(physical association) | 0.670 |
| E | PTPN13 | psi-mi:“MI:0407”(direct interaction) | 0.670 |
| YWHAG | BLTP3B | psi-mi:“MI:0914”(association) | 0.640 |
| YWHAG | BLTP3B | psi-mi:“MI:2364”(proximity) | 0.640 |
| APC | PTPN13 | psi-mi:“MI:0407”(direct interaction) | 0.620 |
| YWHAH | PLEKHG3 | psi-mi:“MI:0914”(association) | 0.610 |
| YWHAB | BLTP3B | psi-mi:“MI:2364”(proximity) | 0.610 |
| FAS | PTPN13 | psi-mi:“MI:0915”(physical association) | 0.590 |
| E | PTPN13 | psi-mi:“MI:0915”(physical association) | 0.590 |
| SLC16A3 | CASK | psi-mi:“MI:0914”(association) | 0.590 |
| YWHAE | PIK3C2A | psi-mi:“MI:0914”(association) | 0.570 |
| YWHAH | BLTP3B | psi-mi:“MI:0914”(association) | 0.570 |
| YWHAZ | PIK3C2A | psi-mi:“MI:0914”(association) | 0.570 |
| YWHAH | BLTP3B | psi-mi:“MI:2364”(proximity) | 0.570 |
| CFTR | PTPN13 | psi-mi:“MI:0407”(direct interaction) | 0.570 |
BioGRID (243): PTPN13 (Affinity Capture-MS), PTPN13 (Affinity Capture-MS), PTPN13 (Affinity Capture-MS), PTPN13 (Affinity Capture-MS), PTPN13 (Co-fractionation), PTPN13 (Proximity Label-MS), PTPN13 (Proximity Label-MS), PTPN13 (Affinity Capture-MS), PTPN13 (Two-hybrid), PLEKHA1 (Affinity Capture-MS), STXBP4 (Affinity Capture-MS), PTPN13 (Proximity Label-MS), PTPN13 (Affinity Capture-MS), PTPN13 (Affinity Capture-MS), KCTD3 (Affinity Capture-MS)
ESM2 similar proteins: A0A571BF63, A0A8M9QN10, A0JMA8, A1A535, A1A5P5, A1L1K1, A2AVJ5, A7YDW0, B3MJV4, B4MV81, O00443, O08576, O17237, Q0V9V7, Q12923, Q14D04, Q17QK1, Q1LYM3, Q2NKQ1, Q3UGY8, Q59EK9, Q5EB20, Q5JWR5, Q5PQS3, Q5R565, Q5RAY1, Q5TH69, Q5U245, Q5U3W3, Q5XHG1, Q61194, Q61QK6, Q64512, Q6ING4, Q6MZQ0, Q6ZUJ8, Q7Z3E5, Q803Q4, Q80U12, Q8BPQ7
Diamond homologs: A0A140LI67, A5PKA5, A7UA95, E1JIT7, O14910, O15018, O19132, O35274, O35867, O35889, O62666, O62674, O62675, O62676, O62677, O62678, O88951, O88952, P11434, P29475, P29476, P31016, P51140, P55196, P57105, P78352, Q07436, Q0P5F3, Q12923, Q14005, Q29498, Q2KIB6, Q32LM6, Q3T0C9, Q3UHD6, Q4KL35, Q5F425, Q5RAA5, Q62108, Q64512
SIGNOR signaling
14 interactions.
| A | Effect | B | Mechanism |
|---|---|---|---|
| PTPN13 | down-regulates | INSR | dephosphorylation |
| PTPN13 | down-regulates | PDCD10 | dephosphorylation |
| PTPN13 | “down-regulates activity” | STK25 | dephosphorylation |
| PTPN13 | “up-regulates quantity by stabilization” | NFKBIA | dephosphorylation |
| PTPN13 | “down-regulates activity” | PDCD10 | dephosphorylation |
| PTPN13 | “up-regulates activity” | EFNB1 | dephosphorylation |
| PTPN13 | “down-regulates activity” | ABL1 | dephosphorylation |
| PTPN13 | “down-regulates activity” | IRS1 | dephosphorylation |
| PTPN13 | “down-regulates activity” | ERBB2 | dephosphorylation |
| PTPN13 | “down-regulates activity” | SRC | dephosphorylation |
| PTPN13 | “down-regulates activity” | TRIP6 | dephosphorylation |
Enriched among interaction partners
Reactome pathways and GO biological processes over-represented among this gene’s 188 IntAct physical interaction partners (hypergeometric vs the genome-wide background, BH-FDR, gene-set size 15–500, ranked by fold). A functional readout of the neighbourhood — distinct from this gene’s own memberships above, and biased toward well-studied / hub proteins, so read it as themes rather than proof.
Reactome pathways:
| Pathway | Partners | Fold | FDR |
|---|---|---|---|
| Chk1/Chk2(Cds1) mediated inactivation of Cyclin B:Cdk1 complex | 8 | 42.3× | 1e-09 |
| Activation of BAD and translocation to mitochondria | 7 | 42.0× | 2e-08 |
| SARS-CoV-1 targets host intracellular signalling and regulatory pathways | 7 | 37.0× | 4e-08 |
| Activation of BH3-only proteins | 7 | 27.4× | 4e-07 |
| RHO GTPases activate PKNs | 8 | 20.0× | 4e-07 |
| EPHA-mediated growth cone collapse | 6 | 18.0× | 4e-05 |
| Intrinsic Pathway for Apoptosis | 7 | 16.1× | 1e-05 |
| FOXO-mediated transcription | 6 | 15.9× | 7e-05 |
GO biological processes:
| GO term | Partners | Fold | FDR |
|---|---|---|---|
| ephrin receptor signaling pathway | 8 | 16.6× | 4e-05 |
| regulation of GTPase activity | 5 | 15.4× | 3e-03 |
| protein targeting | 6 | 13.2× | 1e-03 |
| positive regulation of protein localization to plasma membrane | 7 | 11.5× | 1e-03 |
| Ras protein signal transduction | 7 | 8.7× | 3e-03 |
| positive regulation of neuron projection development | 9 | 7.4× | 1e-03 |
| cell surface receptor protein tyrosine kinase signaling pathway | 7 | 7.3× | 5e-03 |
| intracellular protein localization | 11 | 6.9× | 4e-04 |
Disease & clinical
Cancer significance
From intOGen — cancer-driver classification: loss-of-function (tumor-suppressor-like) across 3 cancer types — BLCA, PANCREAS, UCEC.
Clinical variants and AI predictions
ClinVar
435 variants total. Per-class counts are floors (≥ shown; pagination cap):
| Classification | Count (floor) |
|---|---|
| Pathogenic | 0 |
| Likely pathogenic | 0 |
| Uncertain significance | 348 |
| Likely benign | 25 |
| Benign | 6 |
Top pathogenic / likely-pathogenic (0)
SpliceAI
7392 predictions. Top by Δscore:
| Variant | Effect | Δscore |
|---|---|---|
| 4:86603859:G:GT | donor_gain | 1.0000 |
| 4:86603874:GCCAT:G | donor_gain | 1.0000 |
| 4:86635372:G:A | donor_loss | 1.0000 |
| 4:86635373:T:A | donor_loss | 1.0000 |
| 4:86672336:T:G | acceptor_gain | 1.0000 |
| 4:86672342:A:AG | acceptor_gain | 1.0000 |
| 4:86672342:ATTTT:A | acceptor_gain | 1.0000 |
| 4:86672346:T:TA | acceptor_gain | 1.0000 |
| 4:86672347:G:A | acceptor_gain | 1.0000 |
| 4:86672352:A:AG | acceptor_gain | 1.0000 |
| 4:86672356:A:AG | acceptor_gain | 1.0000 |
| 4:86672357:C:G | acceptor_gain | 1.0000 |
| 4:86672358:A:AG | acceptor_gain | 1.0000 |
| 4:86672359:A:G | acceptor_gain | 1.0000 |
| 4:86672539:AAAAG:A | donor_loss | 1.0000 |
| 4:86672540:AAAGG:A | donor_loss | 1.0000 |
| 4:86672541:AAG:A | donor_loss | 1.0000 |
| 4:86672542:AG:A | donor_loss | 1.0000 |
| 4:86672543:GG:G | donor_loss | 1.0000 |
| 4:86672545:T:A | donor_loss | 1.0000 |
| 4:86686776:G:GG | donor_gain | 1.0000 |
| 4:86686781:T:G | donor_gain | 1.0000 |
| 4:86688998:T:G | acceptor_gain | 1.0000 |
| 4:86689004:GCCT:G | acceptor_gain | 1.0000 |
| 4:86689118:G:GT | donor_gain | 1.0000 |
| 4:86693586:GACA:G | acceptor_gain | 1.0000 |
| 4:86693673:AGG:A | donor_loss | 1.0000 |
| 4:86693674:GGT:G | donor_loss | 1.0000 |
| 4:86693675:G:GC | donor_loss | 1.0000 |
| 4:86693676:T:G | donor_loss | 1.0000 |
AlphaMissense
16339 scored. Top likely-pathogenic:
| Variant | Protein change | am_pathogenicity |
|---|---|---|
| 4:86758951:T:C | L1144S | 1.000 |
| 4:86809811:T:A | W2376R | 1.000 |
| 4:86809811:T:C | W2376R | 1.000 |
| 4:86635338:A:C | S28R | 0.999 |
| 4:86635340:T:A | S28R | 0.999 |
| 4:86635340:T:G | S28R | 0.999 |
| 4:86741787:T:A | W820R | 0.999 |
| 4:86741787:T:C | W820R | 0.999 |
| 4:86759038:T:C | L1173P | 0.999 |
| 4:86764720:T:A | V1382D | 0.999 |
| 4:86766441:T:A | V1418D | 0.999 |
| 4:86769814:G:A | G1512E | 0.999 |
| 4:86769817:T:C | F1513S | 0.999 |
| 4:86807664:G:A | G2284R | 0.999 |
| 4:86807664:G:C | G2284R | 0.999 |
| 4:86809910:A:C | S2409R | 0.999 |
| 4:86809912:T:A | S2409R | 0.999 |
| 4:86809912:T:G | S2409R | 0.999 |
| 4:86734362:T:A | W640R | 0.998 |
| 4:86734362:T:C | W640R | 0.998 |
| 4:86745015:T:C | F846S | 0.998 |
| 4:86758681:T:C | F1106S | 0.998 |
| 4:86758956:T:C | S1146P | 0.998 |
| 4:86766438:G:C | R1417P | 0.998 |
| 4:86766450:T:A | V1421D | 0.998 |
| 4:86766488:G:C | A1434P | 0.998 |
| 4:86767827:T:C | L1447P | 0.998 |
| 4:86769813:G:A | G1512R | 0.998 |
| 4:86769813:G:C | G1512R | 0.998 |
| 4:86769816:T:C | F1513L | 0.998 |
dbSNP variants (sampled 300 via entrez): RS1000009579 (4:86698101 T>A), RS1000011765 (4:86747804 C>A,T), RS1000057006 (4:86624765 A>T), RS1000070988 (4:86641017 G>A,T), RS1000072722 (4:86606120 G>A), RS1000076754 (4:86772436 C>G), RS10000891 (4:86747374 G>A), RS1000096642 (4:86755143 C>A), RS10001010 (4:86747525 G>A), RS1000116504 (4:86701542 C>T), RS1000122749 (4:86714324 T>G), RS1000144132 (4:86598337 G>A,T), RS1000148591 (4:86609009 A>G), RS1000162764 (4:86668337 A>G,T), RS1000164203 (4:86741535 T>C)
Disease associations
OMIM: gene MIM:600267 | disease phenotypes: MIM:156000, MIM:192500
GenCC curated gene-disease
| Disease | Classification | Inheritance |
|---|---|---|
| bone marrow failure syndrome | Moderate | Autosomal recessive |
Mondo (3): Meniere disease (MONDO:0007972), familial long QT syndrome (MONDO:0019171), bone marrow failure syndrome (MONDO:0000159)
Orphanet (3): Romano-Ward syndrome (Orphanet:101016), Congenital long QT syndrome (Orphanet:768), NON RARE IN EUROPE: Menière disease (Orphanet:45360)
HPO phenotypes
0 total (0 of 0 shown, HPO-id order):
GWAS associations
7 associations (top):
| Study | Trait | p-value |
|---|---|---|
| GCST003476_4 | Eyebrow thickness | 2.000000e-06 |
| GCST003861_1 | Kidney disease (end stage renal disease vs normoalbuminuria) in type 1 diabetes | 6.000000e-06 |
| GCST003862_1 | Kidney disease (end stage renal disease vs non-end stage renal disease) in type 1 diabetes | 2.000000e-06 |
| GCST007467_8 | Word spelling | 6.000000e-06 |
| GCST010083_56 | Hemoglobin levels | 1.000000e-08 |
| GCST011541_4 | Tinnitus | 2.000000e-07 |
| GCST90000025_272 | Appendicular lean mass | 6.000000e-23 |
EFO canonical traits (3, from GWAS)
| EFO ID | Trait name |
|---|---|
| EFO:0005301 | reading and spelling ability |
| EFO:0004509 | hemoglobin measurement |
| EFO:0004980 | appendicular lean mass |
MeSH disease descriptors (1)
| Descriptor | Name | Tree numbers |
|---|---|---|
| D008575 | Meniere Disease | C09.218.568.217.500 |
Drugs & pharmacology
Drug and pharmacology data
Is drug target: yes
ChEMBL targets (1): CHEMBL2976 (SINGLE PROTEIN)
PharmGKB: 1 entry (VIP=true, CPIC=false)
ChEMBL bioactivities
17 potent at pChembl≥5 of 29 total, top 17 by pChembl (potency: 10 = 0.1 nM, 6 = 1 µM).
| pChembl | Type | Value | Unit | Molecule |
|---|---|---|---|---|
| 6.41 | IC50 | 390 | nM | CHEMBL2396718 |
| 6.22 | IC50 | 600 | nM | CHEMBL50878 |
| 5.89 | IC50 | 1300 | nM | CHEMBL2316902 |
| 5.80 | IC50 | 1600 | nM | CHEMBL2316907 |
| 5.72 | IC50 | 1900 | nM | CHEMBL2316906 |
| 5.66 | IC50 | 2200 | nM | CHEMBL3985776 |
| 5.55 | IC50 | 2800 | nM | CHEMBL3918902 |
| 5.54 | IC50 | 2900 | nM | CHEMBL2396719 |
| 5.37 | IC50 | 4300 | nM | CHEMBL3979554 |
| 5.36 | IC50 | 4400 | nM | CHEMBL51579 |
| 5.33 | IC50 | 4700 | nM | CHEMBL417727 |
| 5.25 | IC50 | 5600 | nM | CHEMBL3909342 |
| 5.19 | IC50 | 6500 | nM | CHEMBL3900333 |
| 5.16 | IC50 | 7000 | nM | CHEMBL51314 |
| 5.13 | IC50 | 7400 | nM | CHEMBL3899171 |
| 5.00 | IC50 | 9900 | nM | CHEMBL3908861 |
| 5.00 | IC50 | 9900 | nM | CHEMBL50347 |
PubChem BioAssay actives
18 with measured affinity, of 88 total; 18 most potent distinct compounds. Largely complementary to BindingDB; screening values are coarse (µM, 4 dp), so sub-nM hits tie at the floor.
| Compound | Assay | Type | Value | Unit |
|---|---|---|---|---|
| 3-[2-(3-chlorophenyl)ethynyl]-6-hydroxy-2-[4-[2-oxo-2-(propylamino)ethoxy]phenyl]-1-benzofuran-5-carboxylic acid | 755774: Inhibition of recombinant FAP-1 (unknown origin) using pNPP as substrate by spectrophotometric analysis | ic50 | 0.3900 | uM |
| N-(9,10-dioxophenanthren-2-yl)-2-fluorobenzamide | 71463: Inhibitory concentration against FAP-1 pNPP | ic50 | 0.6000 | uM |
| 6-hydroxy-2-phenyl-3-[2-[3-(trifluoromethyl)phenyl]ethynyl]-1-benzofuran-5-carboxylic acid | 725031: Inhibition of FAP1 (unknown origin) expressed in Escherichia coli using pNPP substrate after 5 mins by spectrophotometric analysis | ic50 | 1.3000 | uM |
| 6-hydroxy-2-phenyl-3-[2-[4-(trifluoromethoxy)phenyl]ethynyl]-1-benzofuran-5-carboxylic acid | 725031: Inhibition of FAP1 (unknown origin) expressed in Escherichia coli using pNPP substrate after 5 mins by spectrophotometric analysis | ic50 | 1.6000 | uM |
| 3-[2-(3,5-difluorophenyl)ethynyl]-6-hydroxy-2-phenyl-1-benzofuran-5-carboxylic acid | 725031: Inhibition of FAP1 (unknown origin) expressed in Escherichia coli using pNPP substrate after 5 mins by spectrophotometric analysis | ic50 | 1.9000 | uM |
| 2-[6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-7-hydroxynaphthalen-2-yl]oxy-1-phenothiazin-10-ylethanone | 1322861: Inhibition of recombinant FAP1 (unknown origin) using pNPP as substrate by spectrophotometric method | ic50 | 2.2000 | uM |
| 2-[6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-7-hydroxynaphthalen-2-yl]oxy-N-(4-phenylphenyl)acetamide | 1322861: Inhibition of recombinant FAP1 (unknown origin) using pNPP as substrate by spectrophotometric method | ic50 | 2.8000 | uM |
| 3-[2-(3-chlorophenyl)ethynyl]-2-[4-[2-(cyclopropylamino)-2-oxoethoxy]phenyl]-6-hydroxy-1-benzofuran-5-carboxylic acid | 755774: Inhibition of recombinant FAP-1 (unknown origin) using pNPP as substrate by spectrophotometric analysis | ic50 | 2.9000 | uM |
| (5Z)-3-(3-chlorophenyl)-5-[(4-hydroxy-3-methoxy-5-nitrophenyl)methylidene]-2-sulfanylidene-1,3-thiazolidin-4-one | 1799621: PTP Assay from Article 10.1002/cbic.200600287: “Cellular inhibition of protein tyrosine phosphatase 1B by uncharged thioxothiazolidinone derivatives.” | ic50 | 3.7000 | uM |
| N-[2-(2,4-dichlorophenyl)ethyl]-2-[6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-7-hydroxynaphthalen-2-yl]oxyacetamide | 1322861: Inhibition of recombinant FAP1 (unknown origin) using pNPP as substrate by spectrophotometric method | ic50 | 4.3000 | uM |
| methyl 4-[(9,10-dioxophenanthren-1-yl)amino]-4-oxobutanoate | 71463: Inhibitory concentration against FAP-1 pNPP | ic50 | 4.4000 | uM |
| 2-aminophenanthrene-9,10-dione | 71466: Inhibitory concentration against FAP-1 using pNPP as substrate | ic50 | 4.7000 | uM |
| N-(9H-fluoren-9-yl)-2-[6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-7-hydroxynaphthalen-2-yl]oxyacetamide | 1322861: Inhibition of recombinant FAP1 (unknown origin) using pNPP as substrate by spectrophotometric method | ic50 | 5.6000 | uM |
| 2-[6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-7-hydroxynaphthalen-2-yl]oxy-N-(4-propan-2-ylphenyl)acetamide | 1322861: Inhibition of recombinant FAP1 (unknown origin) using pNPP as substrate by spectrophotometric method | ic50 | 6.5000 | uM |
| N-(9,10-dioxophenanthren-2-yl)-2,2-dimethylpropanamide | 71463: Inhibitory concentration against FAP-1 pNPP | ic50 | 7.0000 | uM |
| N-(1-adamantyl)-2-[6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-7-hydroxynaphthalen-2-yl]oxyacetamide | 1322861: Inhibition of recombinant FAP1 (unknown origin) using pNPP as substrate by spectrophotometric method | ic50 | 7.4000 | uM |
| methyl 8-[(9,10-dioxophenanthren-2-yl)amino]-8-oxooctanoate | 71463: Inhibitory concentration against FAP-1 pNPP | ic50 | 9.9000 | uM |
| N-(1,3-benzothiazol-2-yl)-2-[6-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)-7-hydroxynaphthalen-2-yl]oxyacetamide | 1322861: Inhibition of recombinant FAP1 (unknown origin) using pNPP as substrate by spectrophotometric method | ic50 | 9.9000 | uM |
CTD chemical–gene interactions
64 total (human), top 30 by PubMed support.
| Chemical | Actions (top 5) | PubMed papers |
|---|---|---|
| Valproic Acid | affects cotreatment, decreases expression, affects expression, increases expression | 6 |
| trichostatin A | affects cotreatment, decreases expression | 3 |
| sodium arsenite | increases expression, decreases expression, affects cotreatment, increases abundance | 3 |
| Estradiol | affects cotreatment, increases expression, decreases expression | 3 |
| bisphenol A | decreases methylation, increases expression | 2 |
| potassium chromate(VI) | affects cotreatment, decreases expression, increases expression | 2 |
| (+)-JQ1 compound | increases expression | 2 |
| Arsenic | decreases expression, increases abundance, affects cotreatment | 2 |
| Benzo(a)pyrene | decreases expression, decreases methylation | 2 |
| Tobacco Smoke Pollution | decreases expression, increases expression | 2 |
| Cadmium Chloride | decreases expression, increases abundance | 2 |
| aristolochic acid I | decreases expression | 1 |
| FR900359 | affects phosphorylation | 1 |
| urushiol | increases expression | 1 |
| methylmercuric chloride | decreases expression, increases expression | 1 |
| triphenyl phosphate | affects expression | 1 |
| glycidyl methacrylate | increases expression | 1 |
| sodium arsenate | decreases expression, increases abundance | 1 |
| terbufos | increases methylation | 1 |
| arsenite | affects binding, decreases reaction | 1 |
| doxifluridine | decreases response to substance | 1 |
| manganese chloride | affects cotreatment, decreases expression, increases abundance | 1 |
| LY 117018 | increases expression | 1 |
| cupric oxide | decreases expression | 1 |
| 1-UFT protocol | decreases response to substance | 1 |
| S-(1,2-dichlorovinyl)cysteine | affects cotreatment, decreases expression | 1 |
| epigallocatechin gallate | affects cotreatment, decreases expression | 1 |
| arsenic disulfide | decreases methylation | 1 |
| glycidamide | decreases expression | 1 |
| chromium hexavalent ion | affects expression | 1 |
ChEMBL screening assays
23 unique, capped per target: 22 binding, 1 admet
Representative assays (with source publication via chembl_document):
| Assay ID | Type | Description | Source paper |
|---|---|---|---|
| CHEMBL1070017 | Binding | Inhibition of FAP1 expressed in Escherichia coli assessed as inhibition of p-nitrophenyl phosphate hydrolysis at pH 7 by spectrophotometry | Salicylic acid based small molecule inhibitor for the oncogenic Src homology-2 domain containing protein tyrosine phosphatase-2 (SHP2). — J Med Chem |
| CHEMBL4626300 | ADMET | Inhibition of FAP1 (unknown origin) expressed in Escherichia coli BL21 using p-nitrophenyl phosphate as substrate measured after 30 mins by UV-vis spectrophotometric method | Highly Potent and Selective N-Aryl Oxamic Acid-Based Inhibitors for Mycobacterium tuberculosis Protein Tyrosine Phosphatase B. — J Med Chem |
Cellosaurus cell lines
2 cell lines: 2 cancer cell line
First 10 cell lines (id-ordered, not curated):
| Cellosaurus | Name | Category | Sex |
|---|---|---|---|
| CVCL_B2CS | Abcam HeLa PTPN13 KO | Cancer cell line | Female |
| CVCL_D7YY | Ubigene A-549 PTPN13 KO | Cancer cell line | Male |
Clinical trials (associated diseases)
128 trials via MONDO — disease-level, not drug-specific.
| Trial | Phase | Status | Title |
|---|---|---|---|
| NCT01574313 | PHASE4 | COMPLETED | Effect of Stellate Ganglion Block on Meniere’s Disease |
| NCT02529475 | PHASE4 | TERMINATED | Evaluation of Inner Ear and Brain Structures With Contrast-enhanced MRI in Healthy Subjects (HYDROPS) |
| NCT04815187 | PHASE4 | ACTIVE_NOT_RECRUITING | Repurposed Use of Allergic Rhinitis and Allergic Asthma Drug to Reduce Vertigo and Hearing Loss in Meniere’s Disease |
| NCT02513940 | PHASE4 | COMPLETED | Influence of Testosterone Administration on Drug-Induced QT Interval Prolongation and Torsades de Pointes |
| NCT03834883 | PHASE4 | COMPLETED | Reducing the Risk of Drug-Induced QT Interval Lengthening in Women |
| NCT04169100 | PHASE4 | UNKNOWN | Novel Form of Acquired Long QT Syndrome |
| NCT04675788 | PHASE4 | COMPLETED | Novel Approaches for Minimizing Drug-Induced QT Interval Lengthening |
| NCT00774527 | PHASE3 | COMPLETED | Comparison of Cy-Atg Vs Cy-Flu-Atg for the Conditioning Therapy in Allo-HCT |
| NCT02393508 | PHASE3 | UNKNOWN | The Impact of Red Cell Age on Product Utilization in the Chronically Transfused Outpatient Population |
| NCT06940570 | PHASE3 | SUSPENDED | Methadone as an Alternative Treatment for Children Underdoing HSCT |
| NCT03664674 | PHASE3 | COMPLETED | Phase 3 Study of OTO-104 in Subjects With Unilateral Meniere’s Disease |
| NCT04677972 | PHASE3 | COMPLETED | SPI-1005 for the Treatment of Meniere’s Disease |
| NCT05851508 | PHASE3 | RECRUITING | The Effecttiveness of Intratympanic Methylprednisolon Injections Compared to Placebo in the Treatment of Vertigo Attacks in Meniere’s Disease |
| NCT01050439 | PHASE2 | TERMINATED | Unrelated Donor Transplant for Malignant and Non-Malignant Disorders |
| NCT01596699 | PHASE2 | TERMINATED | Pilot Trial of Clofarabine Added to Standard Busulfan and Fludarabine for Conditioning Prior to Allogeneic Hematopoietic Cell Transplantation |
| NCT01757145 | PHASE2 | UNKNOWN | Eltrombopag for Enhancing Platelet Engraftment in Adult Patients Undergoing Cord Blood Transplantation |
| NCT02224872 | PHASE2 | COMPLETED | Transplantation of Partially Mismatched Related or Matched Unrelated Bone Marrow for Patients With Refractory Severe Aplastic Anemia |
| NCT02277639 | PHASE2 | COMPLETED | Reduced Intensity Conditioning Using CD3+/CD19+ Depletion for Non Malignant Transplantable Diseases |
| NCT02349906 | PHASE2 | COMPLETED | Treosulfan-based Versus Busulfan-based Conditioning in Paediatric Patients With Non-malignant Diseases |
| NCT02722668 | PHASE2 | COMPLETED | UCB Transplant for Hematological Diseases Using a Non Myeloablative Prep |
| NCT04356469 | PHASE2 | RECRUITING | TCR Alpha Beta T-cell Depleted Haploidentical HCT in the Treatment of Non-Malignant Hematological Disorders in Children |
| NCT04558736 | PHASE2 | RECRUITING | Haploidentical HCT for Severe Aplastic Anemia |
| NCT04965597 | PHASE2 | COMPLETED | Treosulfan-Based Conditioning Regimen Before a Blood or Bone Marrow Transplant for the Treatment of Bone Marrow Failure Diseases (BMT CTN 1904) |
| NCT05420350 | PHASE2 | UNKNOWN | Lamotrigine and Bupropion for Meniere’s Disease |
| NCT06544434 | PHASE2 | RECRUITING | Laser Acupuncture for Meniere Disease |
| NCT01648205 | PHASE2 | COMPLETED | Long-term Efficacy Study of Sodium Channel Blocker in LQT3 Patients |
| NCT02412709 | PHASE2 | UNKNOWN | Long QT Syndrome Screening in Newborns |
| NCT04581408 | PHASE2 | COMPLETED | Mutation-specific Therapy for the Long QT Syndrome |
| NCT07585136 | PHASE1 | NOT_YET_RECRUITING | Stem Cell Mobilization and Apheresis for Life-threatening Blood Disorders |
| NCT04674735 | PHASE1 | WITHDRAWN | Safety of APSLXR in Patients Presenting Vertigo of Vestibular Origin or Meniere’s Disease |
| NCT00316459 | PHASE1 | COMPLETED | Study Evaluating the Effects of Multiple Oral Doses of ERB-041 on Cardiac Repolarization in Healthy Subjects |
| NCT01849003 | PHASE1 | COMPLETED | Study of the Effect of GS-6615 in Subjects With LQT-3 |
| NCT02365532 | PHASE1 | COMPLETED | Effect of Oral GS-6615 on Dofetilide-Induced QT Prolongation, Safety, and Tolerability in Healthy Adults |
| NCT02412098 | PHASE1 | COMPLETED | Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Hepatic Function |
| NCT02441829 | PHASE1 | COMPLETED | Pharmacokinetics of Eleclazine in Adults With Normal and Impaired Renal Function |
| NCT05759962 | PHASE1 | COMPLETED | Phase 1 Study of LQT-1213 in Healthy Adults |
| NCT01419704 | PHASE1/PHASE2 | WITHDRAWN | Phase I/II Pilot Study of Mixed Chimerism to Treat Hemoglobinopathies |
| NCT01966367 | PHASE1/PHASE2 | ACTIVE_NOT_RECRUITING | CD34+ (Non-Malignant) Stem Cell Selection for Patients Receiving Allogeneic Stem Cell Transplantation |
| NCT02055456 | PHASE1/PHASE2 | COMPLETED | Nandrolone Decanoate in the Treatment of Telomeropathies |
| NCT02337595 | PHASE1/PHASE2 | COMPLETED | Memory T-cell Infusion to Improve Immunity After TCR-alpha/Beta Depleted Hematopoietic Stem Cell Transplantation |
Related Atlas pages
- Associated diseases: bone marrow failure syndrome
- Disease cohort memberships (association, not causation — diseases whose associated-gene cohort lists this gene; a subset are also under Associated diseases): bone marrow failure syndrome, diabetic kidney disease, familial long QT syndrome, Meniere disease